2-Phenoxy-3-Trichloromethylquinoxalines Are Antiplasmodial Derivatives with Activity against the Apicoplast of
Plasmodium falciparum
apicoplast
quinoxaline
structure-activity relationships
trichloromethyl goup
Journal
Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453
Informations de publication
Date de publication:
26 Jul 2021
26 Jul 2021
Historique:
received:
02
07
2021
revised:
22
07
2021
accepted:
22
07
2021
entrez:
28
8
2021
pubmed:
29
8
2021
medline:
29
8
2021
Statut:
epublish
Résumé
The malaria parasite harbors a relict plastid called the apicoplast. Although not photosynthetic, the apicoplast retains unusual, non-mammalian metabolic pathways that are essential to the parasite, opening up a new perspective for the development of novel antimalarials which display a new mechanism of action. Based on the previous antiplasmodial hit-molecules identified in the 2-trichloromethylquinoxaline series, we report herein a structure-activity relationship (SAR) study at position two of the quinoxaline ring by synthesizing 20 new compounds. The biological evaluation highlighted a hit compound (
Identifiants
pubmed: 34451821
pii: ph14080724
doi: 10.3390/ph14080724
pmc: PMC8400257
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Agence Nationale de la Recherche
ID : ANR-17-CE11-0017
Organisme : Fondation pour la Recherche Médicale
ID : DCM20181039565
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